Phosphorylation and Promising In-Vitro Antimicrobial Activity of Some New Organosulfur Compounds

During the past few decades, interest has been rapidly growing in gaining insight into the properties and transformations of thiosemicarbazide and their derivatives due to their appreciable pharmacological activities. Dimethoxy acetophenone reacts with thiosemicarbazide to afford compound (1). The product allowed to react by fusion with diethylmalonate and ethylacetoacetate to give cyclic compounds (3), (4) and (7). Their products are reacted with triphenylphosphine oxide to produce phosphorylated compounds with four and six membered rings. Some of these products display interesting biological and antibacterial activities which lead to great interest for possible therapeutic uses. The structure of the products are confirmed by elemental analyses, IR, UV, 1H-NMR and MS specra.Â

Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives

In this work, we prepared an excellent yield of (2-oxo-2H-pyrano[3,2-h] quinolin-4-yl) acetic acid; compound (1) and from the reaction of it with hydrazine hydrate (100%) we obtain 2-(2-oxo-2H-pyrano [3,2-h] quinolin-4-yl) aceto hydrazide (2) which is the starting material for the synthesis of several series of new compounds: such as schiff’s bases (3a-e) and compound (4) in good yields, hydrazide derivatives like compound (5), derivatives of mercapto oxadiazole as compound (6) and derivatives of pyrazolyl as compound (7). All these compounds were found to possess high antimicrobial activity against G+ and G- bacteria and against antifungal as described in scheme (1). Anticancer activity was screened only for compound (1). The IC50 value of it against breast cancer was found = 6.83 µM comparable with that of the drug of doxorubicin which has IC50 = 5.6. As a result these newly compounds from (1) to (7) are considerable as potent compounds for various pharmacological activities.Â

Synthesis and Anticancer Activity of Some New Derivatives of Coumarin and Quinolinyl Mercaptotriazoles

Pechmann condensation of ethylacetoacetate with derivatives of phenol by heating in absence of solvent and with montmorillonite clays K-10 afforded coumarin derivatives (1a-e) in good yields which on reaction with thiosemicarbazide in anhydrous pyridine yielded coumarin-quinolinyl mercaptotriazole (2a-e). The latter compounds were evaluated for their antimicrobial and anticancer activities. The newly synthesized compounds were characterized by IR, 1HNMR and mass spectra

A New Type of Synthesis of 1,2,3-Thiadiazole and 1,2,3-Diazaphosphole Derivatives Via-Hurd-Mori Cyclization

We present a short and efficient synthesis of the title compounds starting with cheap and readily available camphor and derivatives of acetophenone. The optimized sequence allows the large-scale preparation of this new type of synthesis in a few steps. New 1,2,3-thiadiazole and 1,2,3-diazaphosphole derivatives 11-20, were prepared from the ketones 1-5 via the corresponding semicarbazones 6-10. The Hurd-Mori and Lalezari methods were used, respectively, for the preparation of these 1,2,3-thiadiazole and 1,2,3-diazaphospholene derivatives. These derivatives exhibit anticancer effect due to their high potential biological activity

Synthesis of Dihydro-and Tetrahydro-1, 2, 4, 5-tetrazines from the Reaction of Nitrilimines with 1-Substituted-1-methylhydrazine

The reaction of nitrilimines (2) with 1-substituted-1-methylhydrazines (3–6) led to the formation of the respective amidrazones (7) when R = CH3, Ph, and to the acyclic adducts (8,9) when R = CHO and COCH3. The acyclic adducts underwent thermal oxidative cyclization at CH3 to give the unexpected 1,2,4,5-tetrazines (10,11). Dihydro-l,2,4,5-tetrazines (12) were also seperated when R = CHO

Reaction of C-aroyl-N-aryl nitrilimines with selected aliphatic keto-hydrazones and keto-methylhydrazones

C-Benzoyl-and C-2-naphthoyl nitrilimines (2) react with methylhydrazones of aliphatic ketones (3, R1= CH3) to afford the cyclocondensation products 1, 2, 4, 5-tetrazines (4, 5). The reaction of simple hydrazones (3, R1= H) with the same nitrilimines gives the acyclic electrophilic addition products (6, 7), rather than the cyclocondensation tetrazine products

1, 2, 4-Triazoles from 1, 3-dipolar cycloaddition reaction of nitrilimines with aliphatic ketohydrazones carrying electron withdrawing groups

Alkanone and cycloalkanone hydrazones (3) carrying electron withdrawing groups (OCOCH3, COCH3, COPh) react with C-benzoyl-and C-2-naphthoylnitrilimines to give the cycloaddition triazole products (6-11). IR, 1H NMR, 13C NMR and mass spectral data are consistent with the assigned triazole ring system. Compounds (8, 9) having an acetyl group, show signal doubling in their 13C NMR spectra, apparently owing to their presence in two different mesomeric structures